U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 621 - 630 of 1215 results

Status:
US Previously Marketed
Source:
Inositol by Commercial Solvents
(1949)
Source URL:
First approved in 1949
Source:
Inositol by Commercial Solvents
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Inositol is a vitamin-like substance. It is found in many plants and animals. It is produced by the human body from glucose, it is not an essential nutrient. Inositol and some of its mono- and polyphosphates function as the basis for a number of signaling and secondary messenger molecules. Inositol is used for diabetic nerve pain, panic disorder, high cholesterol, insomnia, cancer, depression, schizophrenia, Alzheimer’s disease, attention deficit-hyperactivity disorder (ADHD), autism, promoting hair growth, a skin disorder called psoriasis, and treating side effects of medical treatment with lithium. Inositol is also used by mouth for treating conditions associated with polycystic ovary syndrome, including failure to ovulate; high blood pressure; high triglycerides; and high levels of testosterone. Inositol is possibly safe for most adults. It can cause nausea, tiredness, headache, and dizziness.
Sulfamethazine is a sulfonamide used to treat a variety of bacterial diseases in animals. It inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for binding to dihydropteroate synthetase (dihydrofolate synthetase).
Status:
US Previously Marketed
First approved in 1946

Class (Stereo):
CHEMICAL (ACHIRAL)



Trimethadione (brand name is TRIDIONE) is an oxazolidinedione compound that was developed as an antiepileptic agent for control of petit mal seizures that are refractory to treatment with other drugs. Tridione does not modify the maximal seizure pattern in patients undergoing electroconvulsive therapy and has a sedative effect that may increase to the point of ataxia when excessive doses are used. Trimethadione acts as a voltage-activated T-type Ca2+ channel blocker. Trimethadione is rapidly absorbed from the gastrointestinal tract. It is demethylated by liver microsomes to the active metabolite, dimethadione. Approximately 3% of a daily dose of tridione is recovered in the urine as the unchanged drug. The majority of trimethadione is excreted slowly by the kidney in the form of dimethadione.
Dicumarol is an coumarin-like compound found in sweet clover. It is used as oral anticoagulant and acts by inhibiting the hepatic synthesis of vitamin K-dependent coagulation factors (prothrombin and factors VII, IX, and X). It results in decresed prothrombin levels and a decrease in the amount of thrombin generated and bound to fibrin. This reduces the thrombogenicity of clots. Dicumarol is also used in biochemical experiments as an inhibitor of reductases.
Status:
US Previously Marketed
Source:
Pabalate by Robins
(1949)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



AMINOBENZOATE SODIUM is a salt of Aminobenzoic acid. Aminobenzoic acid is an intermediate in the synthesis of folate by bacteria, plants, and fungi. Many bacteria, including those found in the human intestinal tract such as E. coli, generate Aminobenzoic acid from chorismate by the combined action of the enzymes 4-amino-4-deoxychorismate synthase and 4-amino-4-deoxychorismate lyase. Plants produce Aminobenzoic acid in their chloroplasts, and store it as a glucose ester (pABA-Glc) in their tissues. Humans lack the enzymes to convert Aminobenzoic acid to folate, so require folate from dietary sources such as green leafy vegetables. In humans, Aminobenzoic acid is considered nonessential and, although it has been referred to historically as "vitamin Bx", is no longer recognized as a vitamin, because most people have colon bacteria that generate Aminobenzoic acid. The potassium salt is used as a drug against fibrotic skin disorders, such as Peyronie's disease, under the trade name Potaba.
Status:
US Previously Marketed
Source:
Synkayvite by Hoffmann-La Roche
(1941)
Source URL:
First approved in 1941
Source:
Synkayvite by Hoffmann-La Roche
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Menadiol diphosphate is given as a vitamin K supplement to prevent bleeding caused by vitamin K deficiency. Vitamin K is normally obtained from the diet; for example it is found in green leafy vegetables, root vegetables, cereals and dairy products. Although it cannot be made by the human body itself, a certain amount of vitamin K is also made by bacteria that live in the gut. The body normally produces bile to help it absorb fats from the gut. In conditions where there is a problem with the production of bile, for example in certain liver diseases, or if there is a blockage of the bile duct, there can be problems absorbing fats. This can lead to vitamin K deficiency, decreased production of clotting factors and an increased risk of bleeding. In these situations, menadiol diphosphate is given as a vitamin K supplement to increase the production of clotting factors. It is water soluble so is readily absorbed from the gut. Also in 1974 was made attempt to develop tritiated derivatives of Synkavit (menadiol sodium diphosphate, MNDP) of high specific activity as a radioactive drug. Among the 203 evaluable treated cases, some form of response was observed in 23 out of 151 (15·2%) receiving the drug by intravenous injections and 13 out of 52 (25%) after intra-arterial injections. For the sites and types of malignant diseases which showed responses after either intravenous or intra-arterial administration among the 55 patients surviving at least 3 months after the first injection, some form of response was observed in 32 but only 5 of these showed either a "complete" or a "partial" response.It is concluded that further investigation is desirable. Kappadione is a Vitamin K derivative, was discontinued. It was manufactured by Eli Lilly and others Company.
Status:
US Previously Marketed
Source:
Hytakerol by Winthrop-Stearns (Winthrop)
(1940)
Source URL:
First approved in 1940
Source:
Hytakerol by Winthrop-Stearns (Winthrop)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dihydrotachysterol (DHT) is a synthetic vitamin D analog activated in the liver that does not require renal hydroxylation like vitamin D2 (ergocalciferol) and vitamin D3 (cholecalciferol). Dihydrotachysterol is used to treat hypocalcemia, hypoparathyroidism, and prevention of tetany. Dihydrotachysterol is hydroxylated in the liver to 25-hydroxy-dihydrotachysterol, which is the major circulating active form of the drug. Once hydroxylated to 25-hydroxy-dihydrotachysterol, the modified drug binds to the vitamin D receptor. The bound form of the vitamin D receptor serves as a transcriptional regulator of bone matrix proteins, inducing the expression of osteocalcin and suppressing synthesis of type I collagen. Dihydrotachysterol also increases renal phosphate excretion.
Status:
US Previously Marketed
Source:
Kayquinone by Abbott
(1940)
Source URL:
First approved in 1940
Source:
Kayquinone by Abbott
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Menadione, a drug belong to class of Vitamin K, is prescribed for the treatment of hemorrhage, vitamin K deficiency, moderate to severe forms of hypoprothrombinaemia in adults and children. Menadione is a synthetic form of vitamin K, a lipid-soluble vitamin. Vitamin K is a vital cofactor for the biosynthesis of prothrombin, factor VII, IX, X, protein C and protein S. Menadione supports the functions of osteocalcin. Large doses of menadione have been reported to cause adverse outcomes including hemolytic anemia due to glucose-6-phosphate dehydrogenase deficiency, neonatal brain or liver damage, or neonatal death in some rare cases.
Pantothenic acid (known as Vitamin B5) is a water-soluble member of the B-vitamin family that is converted into 4’-phosphopantetheine, which is then converted to co-enzyme A (CoA) via adenosine triphosphate. Pantothenic acid regulates epidermal barrier function and keratinocytes differentiation via CoA metabolism. Pantothenic acid is incorporated into co-enzyme A and protects cells against peroxidative damage by increasing the level of glutathione. A recent feasibility study has also shown that daily oral supplementation of a nutritional agent containing pantothenic acid for 8 weeks was feasible and safe. It was discovered the different pharmacological implementation of pantothenic acid, such as treatment of acne, obesity. Existed some reports, mentioned efficacy using pantothenic acid in systemic lupus erythematosus. Significant reduction in morning stiffness, degree of disability, and severity of pain was reported for persons taking pantothenic acid in case of osteoarthritis and rheumatoid arthritis. Vitamin B5 may increase the effects of a group of drugs called cholinesterase inhibitors, which are used to treat Alzheimer's disease. That might lead to severe side effects.